| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
Reltecimod TFA targets CD28 (T-lymphocyte receptor), a co-stimulatory molecule on T cells. It acts as a CD28 antagonist, inhibiting the CD28/B7-2 co-stimulatory pathway without completely blocking it. By modulating this pathway, it attenuates the inflammatory response to bacterial infections, bacterial exotoxins and endotoxins, and ionizing radiation. It has good resistance to different bacterial infections.
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| ln Vitro |
In vitro, Reltecimod TFA functions as a CD28 antagonist, inhibiting T-cell stimulation by bacterial pathogens. It modulates the inflammatory response by targeting and attenuating the critical CD28/B7-2 co-stimulatory pathway. The compound has beneficial effects against different bacterial infections, their exotoxins and endotoxins.
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| ln Vivo |
Reltecimod (1.25–5 mg/kg; iv) TFA increases the survival rate of mice harboring several bacterial infections [1].
In vivo, Reltecimod TFA has beneficial effects against different bacterial infections, their exotoxins and endotoxins, and ionizing radiation. It is used for the treatment of necrotizing soft tissue infections (NSTI). By inhibiting CD28-mediated T-cell activation, it reduces acute inflammation and improves outcomes in preclinical models of sepsis and bacterial infection. |
| Enzyme Assay |
A cell-free CD28 binding assay can be performed using surface plasmon resonance (SPR). Recombinant CD28-Fc fusion protein is immobilized on a sensor chip. Increasing concentrations of Reltecimod TFA (0.1-1000 nM) are flowed over the chip. Association and dissociation rates are measured, and the Kd value is calculated. Alternatively, an ELISA-based competition assay can be used: plates are coated with CD28, and biotinylated B7-2 is added with varying concentrations of Reltecimod. Binding is detected with streptavidin-HRP.
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| Cell Assay |
Reltecimod TFA is used in cell-based assays to measure T-cell activation. Human peripheral blood mononuclear cells (PBMCs) are isolated from healthy donors and stimulated with anti-CD3 antibody (1 microg/mL) in the presence of varying concentrations of Reltecimod TFA (0.1-1000 nM). After 48-72 h, T-cell proliferation is measured by [3H]-thymidine incorporation or CFSE dilution. Cytokine production (IFN-gamma, IL-2, TNF-alpha) in the supernatant is quantified by ELISA. The compound is expected to reduce T-cell activation and cytokine production.
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| Animal Protocol |
Reltecimod TFA can be studied in mouse models of necrotizing soft tissue infection (NSTI). Female BALB/c mice (6-8 weeks, n=8-10 per group) are injected intramuscularly in the hind limb with a lethal dose of group A Streptococcus (GAS, 1×10⁶ CFU). Two hours post-infection, Reltecimod TFA (1-10 mg/kg, dissolved in PBS) is administered intravenously or intraperitoneally. A control group receives vehicle. Survival is monitored for 10-14 days. Bacterial load in muscle and blood is quantified by CFU plating. Inflammatory cytokine levels (IL-6, TNF-alpha, IL-1beta) in plasma are measured by ELISA. Tissue histology (H&E) is performed to assess necrosis and inflammation.
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| ADME/Pharmacokinetics |
Reltecimod TFA has a molecular weight of 2650-2700 Da (estimated from peptide sequence). It is a white to off-white solid powder. Specific PK parameters have not been reported. As a peptide antagonist, its plasma half-life is expected to be short (minutes to hours) due to proteolytic degradation. The TFA salt enhances solubility. For in vivo use, it can be formulated in PBS or sterile saline.
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| Toxicity/Toxicokinetics |
No detailed toxicity data for Reltecimod TFA are available. In animal studies, the compound was well-tolerated at the doses used (1-10 mg/kg i.v./i.p.) with no overt signs of systemic toxicity. As an immunomodulator, the primary safety concern is immunosuppression and increased susceptibility to infections. However, formal toxicology studies have not been published. Standard safety precautions for handling research peptides should be followed.
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| References | |
| Additional Infomation |
Reltecimod TFA is a research-grade compound and is not approved for clinical use. It is a CD28 antagonist that has been investigated for the treatment of necrotizing soft tissue infections (NSTI). This product is for research use only and not for human therapeutic applications. The TFA salt is the standard commercial form.
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| Molecular Formula |
C46H72N10O15S.XC2HF3O2
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| Molecular Weight |
1037.19 (free base)
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| Related CAS # |
Reltecimod;1447799-33-8
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| Appearance |
White to off-white solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO :~100 mg/mL H2O :< 0.1 mg/mL
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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